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Pimodivir  ≥98%

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包装规格：5mg 10mg 25mg 100mg in glass bottle
溶解性：溶于DMSO（100 mg/mL 超声)
产品描述：基本信息 产品编号：P10667 产品名称：Pimodivir CAS: 1629869-44-8   储存条件 粉末 -20℃ 四年     分子式： C20H19F2N5O2 溶于液体 -80℃ 六个月 分子量 399.39 -20℃ 一个月 化学名：  (2S,3S)-3-((5-fluoro-2-(5-fluoro-1H-pyrrolo[2,3-b]pyridin-3-yl)pyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylic acid   Solubility (25°C)   体外 DMSO 100mg/mL (250.38mM; Need ultrasonic) Ethanol   Water   体内 现配现用   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 2.5038mL 12.5191mL 25.0382mL 5mM 0.5008mL 2.5038mL 5.0076mL 10mM 0.2504mL 1.2519mL 2.5038mL   生物活性 产品描述 一种可口服的甲型流感病毒聚合酶抑制剂，通过抑制PB2亚基起作用。 靶点/IC50 Influenza Virus   体外研究 Pimodivir rescues macrophages from virus-mediated death at non-cytotoxic concentrations 24hpi. The EC50 value for Pimodivir are 8 and 12nM for A(H1N1) and A(H3N2) strains, respectively, whereas the CC50 values are >1μM, giving selectivity indexes (SI) > 125 and > 83 for A(H1N1) and A(H3N2) strains, respectively. Pimodivir significantly attenuates the transcription of viral M1 RNA in macrophages, which are infected with A(H1N1) or A(H3N2) strains for 8 h. Pimodivir inhibits the transcription of viral but not cellular genes. Pimodivir allows some activation of IAV-mediated expression of several cellular genes, which are involved in tryptophan and nucleotide metabolism. Pimodivir possesses excellent anti-IAV but not immuno/metabolo-modulating effect. Pimodivir (VX-787) is very potent against influenza A strains, including pandemic 2009 H1N1 and avian H5N1. Pimodivir (VX-787) shows potent activity against all influenza A virus strains tested, with an EC 50 range of 0.13 to 3.2nM. Pimodivir-selected PB2 variant viruses maintain susceptibility to neuraminidase inhibitors in vitro.   体内研究 Pimodivir (2, 6, and 20mg/kg/day, p.o.) and GS 4071 (20mg/kg/day) completely prevent death in the H1N1pdm virus infection in mice. Pimodivir (20mg/kg/day) is more effective than GS 4071 (20mg/kg/day) in improving body weight and reducing the severity of lung infection. Moreover, Pimodivir (VX-787) shows 100% survival in a +48 h delay to treatment mouse influenza model at 10, 3 and 1mpk (BID × 10 days) whereas the SOC, GS 4071, provide no survival benefit in this model at 10mpk. Pimodivir (VX-787; 1, 3, or 10mg/kg, bid) provided complete survival, with a dose-dependent reduction in BW loss of the mice.   推荐实验方法(仅供参考) 细胞实验:   Cell Assay The compound cytotoxicity and efficacy testing is performed in 96-well plates with macrophages at 95% confluence. The compounds are added to the medium, and 30 min later, the cells are infected with virus or non-infected. The cell viability is analyzed with the Cell Titer Glo assay at 24hpi. The luminescence is read with a PHERAstar FS plate reader   动物实验:   Animal Administration The mice are anesthetized, and the animals are infected intranasally with a 90-μL suspension of influenza virus. The virus challenge is approximately four 50% mouse lethal infectious doses. Treatments are given twice a day (at 12 h intervals) for 10 days starting 2 h before virus challenge. Parameters for assessing the infection are survival, mean day of death, body weight changes, and lung infection parameters (hemorrhage score, weight, and virus titer). Animals are weighed individually every other day through day 21 of the infection. Initially, there are 15 mice per group treated with compound and 25 placebos. Five mice in each group are subsequently sacrificed for determination of lung infection parameters. A larger number of placebos are used than compound-treated mice to achieve greater statistical power, especially if some animals in that group survive the infection. One mouse that dies during the treatment period is presumed to have died from treatment trauma because its death occurs well before other mice die from influenza. It is excluded from the total counts. Animals that die during infection are accounted for in the tabular data.
保存条件：-20℃

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